Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex

Yu Ling Lin, Chia Hung Chen, Hsin Yi Wu, Nu Man Tsai, Ting Yan Jian, Yuan Ching Chang, Chi Hsin Lin, Chih Hsiung Wu, Fei Ting Hsu, Ting Kai Leung*, Kuang-Wen Liao

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


Background: Tamoxifen is currently used for the treatment of both early and advanced estrogen receptor (ER) positive breast cancer in pre- and post-menopausal women. However, using tamoxifen routinely to inhibit endogenous or exogenous estrogen effects is occasionally difficult because of its potential side effects. Objectives: The aim of this study is to design a local drug delivery system to encapsulate tamoxifen for observing their efficacy of skin penetration, drug accumulation and cancer therapy. Methods: A cationic liposome-PEG-PEI complex (LPPC) was used as a carrier for the encapsulation of tamoxifen and forming 'LPPC/TAM' for transdermal release. The cytotoxicity of LPPC/TAM was analyzed by MTT. The skin penetration, tumor growth inhibition and organ damages were measured in xenograft mice following transdermal treatment. Results: LPPC/TAM had an average size less than 270nm and a zeta-potential of approximately 40mV. LPPC/TAM displayed dramatically increased the cytotoxic activity in all breast cancer cells, especially in ER-positive breast cancer cells. In vivo, LPPC drug delivery helped the fluorescent dye penetrating across the skim and accumulating rapidly in tumor area. Administration of LPPC/TAM by transdermal route inhibited about 86% of tumor growth in mice bearing BT474 tumors. This local treatment of LPPC/TAM did not injury skin and any organs. Conclusion: LPPC-delivery system provided a better skin penetration and drug accumulation and therapeutic efficacy. Therefore, LPPC/TAM drug delivery maybe a useful transdermal tool of drugs utilization for breast cancer therapy.

Original languageEnglish
Article number11
JournalJournal of Nanobiotechnology
Issue number1
StatePublished - 19 Feb 2016


  • Breast cancer
  • Lipo-PEG-PEI complex
  • Tamoxifen
  • Transdermal treatment

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